作为缺氧诱导因子-1α脯氨酰羟化酶抑制剂的取代吡啶衍生物的设计与合成
Design and synthesis of substituted pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.
作者信息
Warshakoon Namal C, Wu Shengde, Boyer Angelique, Kawamoto Richard, Sheville Justin, Bhatt Ritu Tiku, Renock Sean, Xu Kevin, Pokross Matthew, Zhou Songtao, Walter Richard, Mekel Marlene, Evdokimov Artem G, East Stephen
机构信息
Lead Discovery, Procter and Gamble Pharmaceuticals, 8700 Mason-Montgomery Rd, Mason, OH 45040, USA.
出版信息
Bioorg Med Chem Lett. 2006 Nov 1;16(21):5616-20. doi: 10.1016/j.bmcl.2006.08.026.
Structure-guided de novo drug design led to the identification of a novel series of substituted pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors. Pyridine carboxyamide derivatives bearing a substituted aryl group at the 5-position of the pyridine ring show appreciable activity, while constraining the side chain by placing a pyrazole carboxylic acid generated a potent lead series with consistent activity against EGLN-1.
基于结构的从头药物设计导致鉴定出一系列新型的取代吡啶衍生物作为缺氧诱导因子-1α脯氨酰羟化酶抑制剂。在吡啶环的5-位带有取代芳基的吡啶甲酰胺衍生物表现出可观的活性，而通过引入吡唑羧酸来限制侧链则产生了一个具有一致的针对EGLN-1活性的有效先导系列。
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